# US 11,026,901 B2 · Treatment or prevention of cardiovascular events via the administration of a colchicine derivative

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- Number: US 11,026,901 B2
- Document ID: US11026901B2
- Status: Granted
- Kind: B2
- Application number: 17/103,683
- Filed: 2020-11-24
- Published: 2021-03-18
- Granted: 2021-06-08
- Earliest claimed: 2012-11-02
- Assignees: Murray and Poole Enterprises Ltd
- Applicants: Murray and Poole Enterprises, LTD.
- Inventors: Mark Nidorf
- Web page: https://patentgrep.com/patent/US11026901B2

## CPC

- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/37: Coumarins, e.g. psoralen
- A61K 31/4365: the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
- A61K 31/616: by carboxylic acids, e.g. acetylsalicylic acid
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A method for the treatment or prevention of a cardiovascular event in a subject with atherosclerotic vascular disease comprising the step of: b) administering a therapeutically effective amount of a compound of formula (I), a known colchicine derivative and/or a salt thereof wherein: R1, R2, R3, R4, R9, R10, R11 and R12 independently represent hydrogen, C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, halogen, C1-4 haloalkyl, nitro, amino, C2-4 acylamino, C1-4 alkyl or dialkylamino, hydroxyl, C1-4 alkoxy, C1-4 alkylthio, a group of the formula —SO2N(Rx)2 or SO2Rx where Rx is C1-4 alkyl, C1-4 acyloxy, or optionally substituted phenyl, optionally substituted phenoxy; R7 and R8 independently represent hydrogen, C1-4 alkyl or C1-4 acyl; and R5′, R5″, R6′ and R6″ independently represent hydrogen, C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, halogen, C1-4 haloalkyl, nitro, amino, C2-4 acylamino, hydroxyl, C1-4 alkoxy or C1-4 alkylthio a group of the formula —SO2N(Rx)2 or SO2Rx where Rx is C1-4 alkyl, C1-4 acyloxy, or optionally substituted phenyl.

## Claims

### Claim 1

A method for treating and/or reducing the risk of acute myocardial infarction in a subject comprising: administering to the subject a therapeutically effective amount of a composition comprising about 0.5 total mg of (i) colchicine, (ii) a salt of (i), or any combination of (i) and (ii), wherein the composition is administered orally and once per day.

### Claim 2 (depends on 1)

The method of claim 1, wherein the composition is administered in the form of a tablet or capsule.

### Claim 3 (depends on 1)

The method of claim 1, wherein the composition is administered in the form of a liquid dose, gel, or powder.

### Claim 4 (depends on 1)

The method of claim 1, wherein the subject has a previous diagnosis of diabetes, past myocardial infarction, unstable angina, coronary bypass surgery, and/or coronary angioplasty.

### Claim 5 (depends on 1)

The method of claim 1, wherein the subject is from about 35 to about 85 years of age.

### Claim 6 (depends on 1)

The method of claim 1, wherein the acute myocardial infarction is non-stent related acute myocardial infarction.

### Claim 7 (depends on 1)

The method of claim 1, wherein the subject is administered the composition daily for at least 24 months.

### Claim 8 (depends on 1)

The method of claim 1, wherein the subject is administered the composition daily for at least 36 months.

### Claim 9 (depends on 1)

The method of claim 1, wherein the subject is administered the composition daily for at least 44 months.

### Claim 10

A method for treating and/or reducing the risk of acute myocardial infarction in a subject comprising: administering to the subject a therapeutically effective amount of a composition comprising no more than about 0.6 total mg of (i) colchicine, (ii) a salt of (i), or any combination of (i) and (ii), wherein the composition is administered orally and once per day.

### Claim 11 (depends on 10)

The method of claim 10, wherein the composition is administered in the form of a tablet or capsule.

### Claim 12 (depends on 10)

The method of claim 10, wherein the composition is administered in the form of a liquid dose, gel, or powder.

### Claim 13 (depends on 10)

The method of claim 10, wherein the subject has a previous diagnosis of diabetes, past myocardial infarction, unstable angina, coronary bypass surgery, and/or coronary angioplasty.

### Claim 14 (depends on 10)

The method of claim 10, wherein the subject is from about 35 to about 85 years of age.

### Claim 15 (depends on 10)

The method of claim 10, wherein the acute myocardial infarction is non-stent related acute myocardial infarction.

### Claim 16 (depends on 10)

The method of claim 10, wherein the subject is administered the composition daily for at least 24 months.

### Claim 17 (depends on 10)

The method of claim 10, wherein the subject is administered the composition daily for at least 36 months.

### Claim 18 (depends on 10)

The method of claim 10, wherein the subject is administered the composition daily for at least 44 months.
